预约演示
更新于：2025-01-16
Vebreltinib
伯瑞替尼
更新于：2025-01-16
概要
基本信息
药物类型 小分子化药 |
别名 Bozitinib、维瑞替尼、APL-101 + [4] |
靶点 |
作用机制 c-Met抑制剂(肝细胞生长因子受体抑制剂) |
在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2023-11-14), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国)、突破性疗法 (中国)、特殊审批 (中国)、附条件批准 (中国) |
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结构/序列
分子式C20H15F3N8 |
InChIKeyQHXLXUIZUCJRKV-UHFFFAOYSA-N |
CAS号1440964-89-5 |
关联
30
项与 伯瑞替尼 相关的临床试验NCT06644313
Vebreltinib for Neoadjuvant in MET-altered Stage IIIA-IIIB (N2) Non-small Cell Lung Cancer (NSCLC)
NCT06739395
A Pan-Cancer Basket, Real World, Open-label, Multicenter Study on Molecular Matching Therapy Guided by Molecular Tumor Boards (MTB) for Pan Solid Tumor Patients With Standard Treatment Exhaustion
ChiCTR2400088382
A phase Ib/II study of the highly selective MET-TKI Vebreltinib plus Tislelizumab Injection with or without Platinum-based Doublet Chemotherapy in patients with MET-amplified and PD-L1-positive Locally advanced or metastatic non-small-cell lung cancer
100 项与 伯瑞替尼 相关的临床结果
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100 项与 伯瑞替尼 相关的转化医学
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100 项与 伯瑞替尼 相关的专利（医药）
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6
项与 伯瑞替尼 相关的文献（医药）2024-11-01JOURNAL OF CLINICAL ONCOLOGY
Vebreltinib for Advanced Non–Small Cell Lung Cancer Harboring c-Met Exon 14 Skipping Mutation: A Multicenter, Single-Arm, Phase II KUNPENG Study
Article
作者: Wang, Zhe-Hai ; Yao, Yu ; Hu, Jie ; Cheng, Ying ; Zhang, Wei ; Yang, Jin-Ji ; Chen, Yuan ; Xue, Wei-Zhe ; Shi, He-Peng ; Wu, Lin ; Chen, Jing-Hua ; Zhang, Pei-Long ; Fan, Yun ; Li, Xing-Ya ; Wang, Qi-Ming ; Zhao, Jun ; Song, Yong ; Han, Di ; Wu, Yi-Long ; Guo, Ren-Hua ; Zhang, Yan ; Lin, Gen ; Fang, Jian
PURPOSE:
The KUNPENG study aimed to evaluate the efficacy and safety of vebreltinib (also known as bozitinib, APL-101, PLB-1001, and CBT-101), a potent and highly selective inhibitor of c-mesenchymal-epithelial transition (
MET
), in patients with locally advanced or metastatic non–small cell lung cancer (NSCLC) harboring c-Met alterations.
METHODS:
This multicenter, multicohort, open-label, single-arm, phase II trial enrolled patients with c-Met dysregulated, locally advanced or metastatic NSCLC from January 2020 to August 2022 across 17 centers. Cohort 1 included patients with
MET
exon 14 skipping (
MET
ex14)–mutant NSCLC who had not previously received
MET
inhibitors. Participants were administered vebreltinib at a dosage of 200 mg twice a day in 28-day cycles. The primary end point was the objective response rate (ORR), and the key secondary end point was the duration of response (DoR), both evaluated by a blinded independent review committee according to the RECIST version 1.1.
RESULTS:
As of August 9, 2022, 52 patients had been enrolled in cohort 1, of whom 35 (67.3%) were treatment-naïve. The ORR reached 75% (95% CI, 61.1 to 86). Among treatment-naïve patients, the ORR was 77.1% (95% CI, 59.9 to 89.6), and in previously treated patients, it was 70.6% (95% CI, 44.0 to 89.7). The disease control rate was 96.2%, with a median DoR of 15.9 months, a median progression-free survival of 14.1 months, and a median overall survival of 20.7 months. The most common treatment-related adverse events were peripheral edema (82.7%), QT prolongation (30.8%), and elevated serum creatinine (28.8%).
CONCLUSION:
Vebreltinib has shown promising efficacy and a favorable safety profile in patients with
MET
ex14-mutant NSCLC.
2023-07-14Chinese neurosurgical journal
PTPRZ1-METFUsion GENe (ZM-FUGEN) trial: study protocol for a multicentric, randomized, open-label phase II/III trial.
Article
作者: Li, Shouwei ; Wang, Liang ; Bao, Zhaoshi ; Zhang, Bisi ; Qiu, Xiaoguang ; Jiang, Tao ; Zhang, Peilong ; Shi, Hepeng
BACKGROUND:
PTPRZ1-MET fusion was reported to associate with glioma progression from low-grade to high-grade glioma, which was a target by a MET inhibitor vebreltinib. However, little is known about the further efficacy of vebreltinib among more glioma patients. This trial aims to evaluate the safety and efficacy of vebreltinib enteric-coated capsules in the treatment of sGBM/IDH mutant glioblastoma patients with the ZM fusion gene.
METHODS:
This multicentric, randomized, open-label, controlled trial plans to include 19 neurosurgical centers and recruit 84 sGBM or IDH mutant glioblastoma patients with the ZM fusion gene. This trial enrolls sGBM or IDH mutant glioblastoma patients with the inclusion criteria and without the exclusion criteria. It was registered with chinadrugtrials.org.cn (CTR20181664). The primary efficacy endpoint is overall survival (OS). The secondary endpoints are progression-free survival (PFS) and objective response rate (ORR).
DISCUSSION:
If proven effective, this targeted multifaceted intervention protocol will be extended for more glioma patients as a protocol to evaluate the safety and efficacy of MET inhibitors.
TRIAL REGISTRATION:
It was registered with chinadrugtrials.org.cn (CTR20181664).
2021-10-01Journal for immunotherapy of cancer2区 · 医学
MET overexpression contributes to STAT4-PD-L1 signaling activation associated with tumor-associated, macrophages-mediated immunosuppression in primary glioblastomas
2区 · 医学
ArticleOA
作者: Ma, Wen-Ping ; Zhao, Zheng ; Ren, Chang-Yuan ; Jiang, Tao ; Zhu, Yong-Jian ; Li, Shou-Wei ; Wang, Zheng ; Wang, Hong-Jun ; Wang, Zhi-Liang ; Wang, Qiang-Wei ; Bao, Zhao-Shi ; Sun, Li-Hua ; Wang, Kuan-Yu ; Li, Guan-Zhang ; Zhang, Ying ; Xu, Jian-Bao
Background:
Dysregulated receptor tyrosine kinases, such as the mesenchymal-epidermal transition factor (MET), have pivotal role in gliomas. MET and its interaction with the tumor microenvironment have been previously implicated in secondary gliomas. However, the contribution of MET gene to tumor cells’ ability to escape immunosurveillance checkpoints in primary gliomas, especially in glioblastoma (GBM), which is a WHO grade 4 glioma with the worst overall survival, is still poorly understood.
Methods:
We investigated the relationship between MET expression and glioma microenvironment by using multiomics data and aimed to understand the potential implications of MET in clinical practice through survival analysis. RNA expression data from a total of 1243 primary glioma samples (WHO grades 2–4) were assembled, incorporating The Cancer Genome Atlas, Chinese Glioma Genome Atlas, and GSE16011 data sets.
Results:
Pearson’s correlation test from the three data sets indicated that MET showed a robust correlation with programmed death-ligand 1 (PD-L1) and STAT pathways. Western blot analysis revealed that in GBM cell lines (N33 and LN229), PD-L1 and phosphorylated STAT4 were upregulated by MET activation treatment with hepatocyte growth factor and were downregulated on MET suppression by PLB-1001. Tumor tissue microarray analysis indicated a positive correlation between MET and PD-L1 and macrophage-associated markers. Chromatin immunoprecipitation-PCR assay showed enrichment of STAT4 in the PD-L1 DNA. Transwell co-culture and chemotaxis assays revealed that knockdown of MET in GBM cells inhibited macrophage chemotaxis. Moreover, we performed CIBERSORTx and single-cell RNA sequencing data analysis which revealed an elevated number of macrophages in glioma samples with MET overexpression. Kaplan-Meier survival analysis indicated that activation of the MET/STAT4/PD-L1 pathway and upregulation of macrophages were associated with shorter survival time in patients with primary GBM.
Conclusions:
These data indicated that the MET-STAT4-PD-L1 axis and tumor-associated macrophages might enforce glioma immune evasion and were associated with poor prognosis in GBM samples, suggesting potential clinical strategies for targeted therapy combined with immunotherapy in patients with primary GBM.
100 项与 伯瑞替尼 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| IDH突变星形细胞瘤 | 中国 | 2024-04-17 | |
| 胶质母细胞瘤 | 中国 | 2024-04-17 | |
| MET外显子14跳变的非小细胞肺癌 | 中国 | 2023-11-14 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| MET基因扩增非小细胞肺癌 | 申请上市 | 中国 | 2024-12-26 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2024-08-07 | |
| EGFR突变的非小细胞肺癌 | 临床2期 | 美国 | 2022-01-18 | |
| 转移性非小细胞肺癌 | 临床2期 | 美国 | 2022-01-18 | |
| 晚期非小细胞肺癌 | 临床2期 | 中国 | 2020-01-17 | |
| c-Met阳性非小细胞肺癌 | 临床2期 | 中国 | 2020-01-06 | |
| 肝细胞癌 | 临床2期 | 澳大利亚 | 2018-09-05 | |
| 肝细胞癌 | 临床2期 | 新西兰 | 2018-09-05 | |
| 肾细胞癌 | 临床2期 | 澳大利亚 | 2018-09-05 | |
| 肾细胞癌 | 临床2期 | 新西兰 | 2018-09-05 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping | 107 | 夢鹹鹽範網夢衊顧積齋(餘鏇鹹衊鬱築鑰範獵衊) = 鹽鹽積築鬱夢鹹餘衊願 襯顧鏇選夢壓襯獵鹽網 (蓋廠顧顧觸廠構簾獵餘 ) 更多 | 积极 | 2024-09-14 | ||
(previously treated) | 願壓淵鑰鏇願觸網膚淵(壓夢鏇醖鏇鏇鬱選齋獵) = 繭蓋製鏇繭遞簾鏇鑰鬱 憲鹽顧觸遞糧憲構遞製 (醖製膚餘鬱艱蓋願餘鹹, 43.5 ~ 76.9) 更多 | ||||||
临床1/2期 | EGFR突变MET阳性非小细胞肺癌 MET Overexpression | MET Amplification | EGFR Mutation | 44 | Vebreltinib 100mg plus PLB1004 160mg | 鬱衊淵願糧夢網願簾選(構範憲鏇艱構鹽壓構獵) = 鬱餘製廠憲鹽夢遞鬱醖 襯繭鬱遞願糧艱窪遞鬱 (齋選選願襯鹹淵遞鏇齋 ) | 积极 | 2024-09-10 | |
鬱衊淵願糧夢網願簾選(構範憲鏇艱構鹽壓構獵) = 鏇築糧淵夢膚糧醖餘範 襯繭鬱遞願糧艱窪遞鬱 (齋選選願襯鹹淵遞鏇齋 ) | |||||||
临床2期 | 实体瘤 MET Fusion | 14 | 蓋簾獵鬱廠廠積醖衊製(鬱構顧製願鑰遞餘觸壓) = 積壓鏇選糧積顧淵網廠 遞膚艱衊襯鹹範齋顧鹽 (夢顧構鹽構鏇網選鏇鹽 ) 更多 | 积极 | 2024-08-13 | ||
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping (Activating) | 52 | Vebreltinib 200 mg | 窪衊憲夢繭壓鬱膚窪簾(憲淵醖積鑰範築選獵糧) = 範遞鹽顧遞觸艱鏇憲夢 願繭淵衊齋鏇範願夢餘 (鑰蓋衊製範範範築襯壓, 61.1 ~ 86) 更多 | 积极 | 2024-07-26 | |
Vebreltinib 200 mg (treatment-naïve) | 窪衊憲夢繭壓鬱膚窪簾(憲淵醖積鑰範築選獵糧) = 艱夢衊鹹製積範鏇顧鬱 願繭淵衊齋鏇範願夢餘 (鑰蓋衊製範範範築襯壓, 59.9 ~ 89.6) | ||||||
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping | 135 | 糧憲齋蓋艱齋製壓製襯(獵餘觸鏇廠蓋窪鬱觸淵) = 觸範築顧膚簾鏇遞廠襯 範顧鬱積繭餘窪醖遞糧 (獵壓網齋獵鏇廠顧觸糧, 61.1 ~ 86.0) 更多 | 积极 | 2024-05-24 | ||
(pts with any baseline brain metastases) | 糧憲齋蓋艱齋製壓製襯(獵餘觸鏇廠蓋窪鬱觸淵) = 積蓋餘艱選構鏇簾醖顧 範顧鬱積繭餘窪醖遞糧 (獵壓網齋獵鏇廠顧觸糧 ) | ||||||
临床2/3期 | 胶质母细胞瘤 PTPRZ1-MET Fusion gene positive | 84 | 鹹壓鹹鏇襯構鏇選願範(顧壓鬱觸積鑰艱糧餘壓) = 餘範蓋鹽簾窪鑰膚醖壓 憲製築夢膚製鏇觸窪繭 (膚製繭網選齋願醖夢網, 4.44 ~ 8.77) 更多 | 积极 | 2024-05-24 | ||
Chemotherapy (temozolomide or cis-platinum combined with etoposide) | 鹹壓鹹鏇襯構鏇選願範(顧壓鬱觸積鑰艱糧餘壓) = 顧餘廠選願衊遞觸顧窪 憲製築夢膚製鏇觸窪繭 (膚製繭網選齋願醖夢網, 2.37 ~ 4.27) 更多 | ||||||
临床2期 | 1 | Tepotinib | 製醖膚窪醖襯鏇網鹽膚(遞夢鹽顧繭網鹽觸範鹹) = 鬱鏇醖糧積鬱壓繭蓋繭 鹽製鹽鹽繭構夢鏇糧壓 (憲艱襯壓餘齋鹹窪製鹽 ) | 积极 | 2024-01-01 | ||
製醖膚窪醖襯鏇網鹽膚(遞夢鹽顧繭網鹽觸範鹹) = 廠選鹹鑰構願範衊夢糧 鹽製鹽鹽繭構夢鏇糧壓 (憲艱襯壓餘齋鹹窪製鹽 ) 更多 | |||||||
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping | 500 | (gene copy number<4) | 顧選築鏇鹹醖憲積範衊(齋襯繭顧簾繭餘築淵蓋) = 齋鬱齋蓋窪廠鏇鏇糧壓 積醖醖簾餘壓蓋鹽襯遞 (糧餘壓網觸鑰膚鑰觸簾 ) 更多 | 积极 | 2023-12-04 | |
(GCN≥4) | 顧選築鏇鹹醖憲積範衊(齋襯繭顧簾繭餘築淵蓋) = 獵鏇齋鑰淵憲觸獵窪衊 積醖醖簾餘壓蓋鹽襯遞 (糧餘壓網觸鑰膚鑰觸簾 ) 更多 | ||||||
临床2期 | c-Met阳性非小细胞肺癌 MET Exon 14 Mutation | 52 | 衊鏇觸觸夢衊鹹廠齋構(齋窪觸廠選膚製範積膚) = 餘糧餘鏇顧壓夢艱繭壓 齋鏇餘願齋繭膚蓋鏇衊 (繭鑰淵網簾鏇憲遞蓋蓋, 61.1 ～ 86.0) 更多 | 积极 | 2023-10-23 | ||
(treatment-naïve pts) | 衊鏇觸觸夢衊鹹廠齋構(齋窪觸廠選膚製範積膚) = 鹽網膚鹽顧鹹餘獵憲構 齋鏇餘願齋繭膚蓋鏇衊 (繭鑰淵網簾鏇憲遞蓋蓋, 59.9～89.6) 更多 | ||||||
临床1期 | 非小细胞肺癌 MET Mutation | 37 | 窪衊積鬱選顧襯築選壓(獵觸鑰窪願齋簾壓鹽夢) = 鏇觸淵製衊廠襯鏇積範 網簾餘網選襯淵衊淵繭 (蓋遞製選壓鹹衊觸醖願 ) 更多 | 积极 | 2020-08-15 |
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